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Study of mutagenic activity of troxerutin, a flavonoid derivative
Abstract:
Troxerutin, a flavonoid derivative, used in vascular diseases was studied in 4 mutagenicity tests: the Ames test, the point mutation test (V79/HPRT), the in vitro metaphase analysis in human lymphocytes and the micronucleus test in mice. The aglycone trihydroxyethylquercetin (THEQ) and quercetin were studied too. Troxerutin was not mutagenic, whereas quercetin was positive in the Ames test, V79 cells and in vitro metaphase analysis. THEQ was negative in the Ames test. The substitution of quercetin with hydroxyethyl groups in 7,3' and 4' positions abolished mutagenic activity of quercetin.
Insights
Troxerutin, a flavonoid derivative, showed no mutagenic activity in four tests. In contrast, quercetin demonstrated mutagenicity, which was abolished by hydroxyethyl group substitution.
Area of Science:
- Biochemistry
- Toxicology
- Pharmacology
Background:
- Troxerutin is a flavonoid derivative used for vascular diseases.
- Flavonoids, like quercetin, can exhibit varying biological activities, including potential mutagenicity.
- Understanding the genotoxic profile of Troxerutin and related compounds is crucial for safety assessment.
Purpose of the Study:
- To evaluate the mutagenicity of Troxerutin.
- To compare the mutagenic potential of Troxerutin with quercetin and its aglycone, trihydroxyethylquercetin (THEQ).
- To investigate the role of hydroxyethyl group substitution in modulating quercetin's mutagenicity.
Main Methods:
- Ames test for bacterial reverse mutation.
- V79/HPRT assay for gene mutation in mammalian cells.
- In vitro metaphase analysis of human lymphocytes for chromosomal aberrations.
- In vivo micronucleus test in mice for genotoxicity.
Main Results:
- Troxerutin was found to be non-mutagenic across all four tested assays.
- Quercetin tested positive for mutagenicity in the Ames test, V79 cells, and in vitro metaphase analysis.
- Trihydroxyethylquercetin (THEQ) was negative in the Ames test.
- Substitution of quercetin with hydroxyethyl groups at the 7, 3', and 4' positions eliminated its mutagenic activity.
Conclusions:
- Troxerutin does not possess mutagenic properties.
- The genotoxicity of quercetin is significantly reduced or abolished by hydroxyethylation.
- Troxerutin is a safer alternative to quercetin concerning mutagenic potential.